| Bioactivity | MRS2365 is a potent and selective P2Y1 receptor (EC50=0.4 nM) /[35S]GTPγS binding/β-arrestin 2 recruitment agonist with an EC50 of 0.4 nM. MRS2365 relieves mechanical allodynia and increases mechanical sensitivity. MRS2365 shows little agonist or antagonist activity at the P2Y12 or P2Y13 receptors[1][2][3][4]. |
| Invitro | MRS2365 (1 µM 或 3 µM；2 min) 弱化了腺苷二磷酸 (ADP) 诱导的血小板聚集[2]。 |
| In Vivo | MRS2365 (0.03-0.3 mg/kg；腹腔注射；单剂量) 以剂量依赖性方式显著减轻雄性 wistar 大鼠神经病变 (Seltzer) 模型中的机械异常性疼痛[3]。MRS2365 (0.1-2 mg/kg；腹腔注射；单剂量) 增加了患有神经性疼痛的雄性 wistar 大鼠模型的缩爪阈值 (PWT) [3]。 Animal Model: |
| Name | MRS2365 |
| CAS | 436847-09-5 |
| Formula | C13H19N5O9P2S |
| Molar Mass | 483.33 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Mariya Chhatriwala, et al. Induction of novel agonist selectivity for the ADP-activated P2Y1 receptor versus the ADP-activated P2Y12 and P2Y13 receptors by conformational constraint of an ADP analog. J Pharmacol Exp Ther. 2004 Dec;311(3):1038-43. [2]. D M Bourdon, et al. (N)-methanocarba-2MeSADP (MRS2365) is a subtype-specific agonist that induces rapid desensitization of the P2Y1 receptor of human platelets. J Thromb Haemost. 2006 Apr;4(4):861-8. [3]. Andó RD, et al. A comparative analysis of the activity of ligands acting at P2X and P2Y receptor subtypes in models of neuropathic, acute and inflammatory pain. Br J Pharmacol. 2010 Mar;159(5):1106-17. [4]. Gao ZG, et al. Distinct Signaling Patterns of Allosteric Antagonism at the P2Y1 Receptor. Mol Pharmacol. 2017 Nov;92(5):613-626. |